Non-nucleoside reverse transcriptase inhibitors

US6716850B2 · kind B2 · utility

Assignee

• MEDIVIR AB · SE

Inventors

• Stefan Lindstrom · Huddinge, SE
• Christer Sahlberg · Stuvsta-Snättringe, SE
• Hans Wallberg · Stuvsta-Snättringe, SE
• Genaidy Kalyanov · Stuvsta-Snättringe, SE
• Lourdes Salvador ODEN · Huddinge, SE
• Lotta Naeslund · Uppsala, SE

Key dates

• Filing date: Mar 5, 2002
• Grant date: Apr 6, 2004
• Expiry date: Aug 2, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the formula I: where;R1 is O, S;R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond;R3 is H, C1-C3 alkyl,R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto;X is —(CHR8)n-—D—(CHR8)m—;D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—;R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl;R9 is H, C1-C3 alkyl;n and m are independently 0, 1 or 2;and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.